Product Information
Registration Status: ActiveZOMIG RAPIMELT TABLET 2.5mg is approved to be sold in Singapore with effective from 2002-02-22. It is marketed by ASTRAZENECA SINGAPORE PTE LTD, with the registration number of SIN11816P.
This product contains Zolmitriptan 2.5mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by CIMA LABS INCCephalon Inc. in UNITED STATES.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water.
Indication
For the acute treatment of adult migraine with or without auras.
Mechanism of Action
Zolmitriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
Pharmacokinetics
- Absorption
- Mean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption.
- Distribution
- * 8.4±3.3 L/kg
- Metabolism
- Hepatic. There have been three metabolites identified: indole acetic acid, N -oxide, and N-desmethyl metabolites. However, the N-desmethyl is the only active metabolite.
- Elimination
Clearance
* 25.9 mL/min/kg
Active Ingredient/Synonyms
(S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one | 311C90 | 4-[[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]methyl]oxazolidin-2-one | Zolmitriptan | Zolmitriptanum | Zolmitriptan |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.